BG104933A - Водоразтворими азоли като антифунгали с широк спектър на действие - Google Patents

Водоразтворими азоли като антифунгали с широк спектър на действие

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Publication number
BG104933A
BG104933A BG104933A BG10493300A BG104933A BG 104933 A BG104933 A BG 104933A BG 104933 A BG104933 A BG 104933A BG 10493300 A BG10493300 A BG 10493300A BG 104933 A BG104933 A BG 104933A
Authority
BG
Bulgaria
Prior art keywords
radical
4alkyl
hydrogen
represents hydrogen
het1
Prior art date
Application number
BG104933A
Other languages
English (en)
Other versions
BG64954B1 (bg
Inventor
Lieven Meerpoel
Leo Jacobus Jozef Backx
Der Veken Louis Van
Frank Christopher Odds
Jan Heeres
Original Assignee
Janssen Pharmaceutica N.V.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of BG104933A publication Critical patent/BG104933A/bg
Publication of BG64954B1 publication Critical patent/BG64954B1/bg

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/12—Oxygen or sulfur atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Изобретението се отнася до нови съединения с формула до техните N-оксидни форми, до техни фармацевтично приемливи присъединителни соли и стереохимични изомерни форми. Във формулата L представлява радикал с формули@@в които всеки Alк независимо представлява заместен по избор С1-6 алкандиил; n има стойност 1, 2 или 3; Y e О, S или NR2; R1 представлява водород, арил, Xem1 или заместен по избор С1-6 алкил; всеки R2 независимо представлява водород или С1-6 алкил; или в случаите, когато R1 и R2 са прикрепени към един и същи азотен атом, те заедно образуват хетероциклен радикал или азидорадикал; всеки R3 независимо означава водород, хидрокси, или С1-4 алкилокси; арил представлява фенил, нафталенил, 1,2,3,4-тетрахидронафталенил, инденил или инданил; всяка една от посочените арилови групи може дабъде заместена по избор; Хеm1 е по избор заместенмоноциклен или бициклен хетероциклен радикал; Xem2 има значение като Xem1 и може също така да бъде пиперазинил, хомопиперазинил, 1,4-диоксанил, морфолинил, тиоморфолинил; R6 означава водород, или С1-4 алкил; R7 е водород или С1-4 алкил; или R6 и R7,взети заедно, образуват бивалентен радикал -N=CH-(i), -CH=N- (ii), -CH=CH- (iii), -CH2-CH2 (iv),където един водороден атом в радикалите (i) и (ii) може да се замести с С1-4 алкилов радикал и един или повече водородни атоми в радикали (iii) и (iv) могат да се заместят с С1-4 алкилов радикал; D означава тризаместено 1,3-диоксоланово производно. Изобретението се отнася също до приложението
BG104933A 1998-05-14 2000-11-09 Водоразтворими азоли като антифунгали с широк спектър на действие BG64954B1 (bg)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP98201588A EP0957101A1 (en) 1998-05-14 1998-05-14 Water soluble azoles as broad-spectrum antifungals

Publications (2)

Publication Number Publication Date
BG104933A true BG104933A (bg) 2001-10-31
BG64954B1 BG64954B1 (bg) 2006-10-31

Family

ID=8233724

Family Applications (2)

Application Number Title Priority Date Filing Date
BG104717A BG64388B1 (bg) 1998-05-14 2000-08-28 Водоразтворими азоли като антифунгали с широк спектър на действие
BG104933A BG64954B1 (bg) 1998-05-14 2000-11-09 Водоразтворими азоли като антифунгали с широк спектър на действие

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BG104717A BG64388B1 (bg) 1998-05-14 2000-08-28 Водоразтворими азоли като антифунгали с широк спектър на действие

Country Status (32)

Country Link
US (2) US6384030B1 (bg)
EP (3) EP0957101A1 (bg)
JP (2) JP2002514646A (bg)
KR (2) KR100593395B1 (bg)
CN (2) CN1137118C (bg)
AR (2) AR016480A1 (bg)
AT (2) ATE221884T1 (bg)
AU (2) AU751135B2 (bg)
BG (2) BG64388B1 (bg)
BR (2) BR9911057A (bg)
CA (2) CA2331141C (bg)
CO (1) CO5021227A1 (bg)
CZ (2) CZ298702B6 (bg)
DE (2) DE69902461T2 (bg)
DK (1) DK1077976T3 (bg)
EE (2) EE04311B1 (bg)
ES (2) ES2198915T3 (bg)
HK (2) HK1033312A1 (bg)
HR (2) HRP20000741B1 (bg)
HU (2) HUP0103536A3 (bg)
IL (2) IL139649A (bg)
MY (2) MY122147A (bg)
NO (2) NO319760B1 (bg)
NZ (2) NZ507966A (bg)
PL (2) PL194086B1 (bg)
PT (1) PT1077976E (bg)
SI (1) SI1077976T1 (bg)
SK (2) SK286156B6 (bg)
TR (2) TR200003322T2 (bg)
TW (2) TW572899B (bg)
WO (2) WO1999058530A1 (bg)
ZA (2) ZA200007173B (bg)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0957101A1 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals
NZ521241A (en) * 2000-03-07 2004-02-27 Ranbaxy Lab Ltd Azole compounds as therapeutic agents for fungal infections
EP1413301A1 (fr) * 2002-10-24 2004-04-28 Bayer CropScience SA Médicaments antifongiques à base de dérivés d'arylamidine
ITMI20032020A1 (it) 2003-10-17 2005-04-18 Italfarmaco Spa Nuovi agenti antifungini azolici con diminuita interazione con i citocromi metabolici
AR052342A1 (es) * 2004-12-21 2007-03-14 Janssen Pharmaceutica Nv Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores
BR112012029227B1 (pt) * 2010-05-19 2020-01-07 Sandoz Ag Processo para a preparação de um composto quiral, composto quiral e uso de um composto
US9346791B2 (en) 2011-09-07 2016-05-24 The Johns Hopkins University Itraconazole analogs and use thereof
US11028078B2 (en) 2011-09-07 2021-06-08 The Johns Hopkins University Itraconazole analogs and use thereof
JP6414831B2 (ja) 2013-06-07 2018-10-31 ザ カリフォルニア インスティテュート フォー バイオメディカル リサーチ 繊維症の小分子阻害剤
WO2016087880A1 (en) 2014-12-05 2016-06-09 Pulmocide Limited Antimycotic compound
US10336735B2 (en) 2014-12-10 2019-07-02 The Scripps Research Institute Small molecule inhibitors of fibrosis
CA2981945C (en) * 2015-05-21 2023-08-29 Pulmocide Limited Antifungal 4-(4-(4-(((3r,5r)-5-((1 h-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)-3-methylphenyl)piperazin-1-yl)-n-(2-hydroxycyclohexyl) benzamide, or a pharmaceutically acceptable salt thereof
CN105237392B (zh) * 2015-11-24 2017-12-12 辽宁渤大化工有限公司 芳烷基水杨酸及其衍生物的制备方法
US11390613B2 (en) 2017-08-20 2022-07-19 University Of Connecticut Azole analogues and methods of use thereof
CN111138421A (zh) * 2019-12-26 2020-05-12 上海英诺富成生物科技有限公司 抗真菌水溶性化合物及其制备方法与应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4267179A (en) * 1978-06-23 1981-05-12 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
PL172358B1 (en) * 1992-03-18 1997-09-30 Janssen Pharmaceutica Nv Stereoisomeric form of itraconazole or saperconazole and method of obtaining same
WO1995017407A1 (en) * 1993-12-21 1995-06-29 Schering Corporation Tetrahydrofuran antifungals
KR100352147B1 (ko) * 1994-01-24 2002-11-11 얀센 파마슈티카 엔.브이. 수용성아졸항진균제
FI98688C (fi) * 1994-07-20 1997-07-25 Nokia Telecommunications Oy Menetelmä lyhytsanomalähetyksen käynnistämiseksi solukkoradiojärjestelmässä, solukkoradiojärjestelmä sekä solukkoradiojärjestelmän tilaajarekisteri
NZ309281A (en) * 1995-06-02 1998-07-28 Schering Corp (2r-cis)-4-[4-[4-[4-[[(5-(2,4-dihalophenyl)-tetrahydro-5-(1h-1,2,4-tr iazol-1-ylmethyl)-tetrahydrofuran-3-yl]methoxy]phenyl]2,4-dihydro-2-[ esters and ethers of mono- or dihydroxy-substituted (c4-c5) alkyl]-3h-1,2,4-triazol-3-one
EP0837859B1 (en) * 1995-06-19 2003-08-13 Schering Corporation Tetrahydrofuran antifungals
BR9809744A (pt) * 1997-02-11 2000-06-20 Janssen Pharmaceutica Nv Antifúngicos de azol contendo éster de aminoácido
EP0957101A1 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals

Also Published As

Publication number Publication date
NO20005712D0 (no) 2000-11-13
SI1077976T1 (en) 2003-02-28
IL139649A0 (en) 2002-02-10
US6448244B1 (en) 2002-09-10
AU4361599A (en) 1999-11-29
NO20005712L (no) 2000-12-07
BG64954B1 (bg) 2006-10-31
ATE221884T1 (de) 2002-08-15
WO1999058529A1 (en) 1999-11-18
SK285763B6 (sk) 2007-07-06
EP1077976A1 (en) 2001-02-28
CA2331141A1 (en) 1999-11-18
BG104717A (bg) 2001-07-31
HK1033312A1 (en) 2001-08-24
CN1300287A (zh) 2001-06-20
KR100593395B1 (ko) 2006-06-28
NO319760B1 (no) 2005-09-12
TW572899B (en) 2004-01-21
EP1077976B1 (en) 2002-08-07
CN1137118C (zh) 2004-02-04
EP1077975B1 (en) 2003-04-23
PL344037A1 (en) 2001-09-24
ES2182531T3 (es) 2003-03-01
PL194086B1 (pl) 2007-04-30
CA2331187A1 (en) 1999-11-18
PL194085B1 (pl) 2007-04-30
AR016482A1 (es) 2001-07-04
IL139647A0 (en) 2002-02-10
EE200000651A (et) 2002-04-15
ES2198915T3 (es) 2004-02-01
AU751135B2 (en) 2002-08-08
BR9911057A (pt) 2001-02-06
HRP20000741A2 (en) 2001-06-30
EE04311B1 (et) 2004-06-15
CN1300288A (zh) 2001-06-20
EP0957101A1 (en) 1999-11-17
EP1077975A1 (en) 2001-02-28
ZA200007459B (en) 2002-09-13
CA2331141C (en) 2008-10-28
CZ20004109A3 (en) 2001-05-16
NO20005713L (no) 2001-01-11
PL344047A1 (en) 2001-09-24
SK16812000A3 (sk) 2001-08-06
KR20010041480A (ko) 2001-05-25
TR200003322T2 (tr) 2001-02-21
MY122147A (en) 2006-03-31
PT1077976E (pt) 2002-12-31
EE200000657A (et) 2002-04-15
HUP0103536A3 (en) 2002-08-28
AU4141799A (en) 1999-11-29
WO1999058530A1 (en) 1999-11-18
DE69907171T2 (de) 2004-02-05
EE04346B1 (et) 2004-08-16
BR9910448A (pt) 2001-01-02
TR200003323T2 (tr) 2001-02-21
ZA200007173B (en) 2002-03-04
CO5021227A1 (es) 2001-03-27
DE69902461T2 (de) 2003-04-10
CA2331187C (en) 2008-11-18
AU758876B2 (en) 2003-04-03
HUP0102031A2 (hu) 2002-05-29
HRP20000740A2 (en) 2001-10-31
BG64388B1 (bg) 2004-12-30
HK1032781A1 (en) 2001-08-03
DE69907171D1 (de) 2003-05-28
MY120248A (en) 2005-09-30
NO319851B1 (no) 2005-09-19
IL139649A (en) 2004-09-27
US6384030B1 (en) 2002-05-07
CZ20004108A3 (en) 2001-05-16
HUP0103536A2 (hu) 2002-07-29
KR20010042852A (ko) 2001-05-25
HRP20000740B1 (en) 2003-12-31
SK286156B6 (sk) 2008-04-07
AR016480A1 (es) 2001-07-04
NZ507965A (en) 2002-05-31
NO20005713D0 (no) 2000-11-13
ATE238296T1 (de) 2003-05-15
CZ298702B6 (cs) 2007-12-27
HRP20000741B1 (en) 2009-02-28
CN1135229C (zh) 2004-01-21
NZ507966A (en) 2002-10-25
TWI259835B (en) 2006-08-11
JP2002514645A (ja) 2002-05-21
CZ299481B6 (cs) 2008-08-13
JP2002514646A (ja) 2002-05-21
DK1077976T3 (da) 2002-12-02
DE69902461D1 (de) 2002-09-12
KR100575147B1 (ko) 2006-05-03
SK16822000A3 (sk) 2001-07-10
HUP0102031A3 (en) 2002-10-28

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